Y. Tauchi et al., Inhibitory effect of dexamethasone palmitate-low density lipoprotein complex on low density lipoprotein-induced macrophage foam cell formation, BIOL PHAR B, 23(4), 2000, pp. 466-471
We used low density lipoprotein (LDL) as a carrier of site-specific deliver
y of drugs to atherosclerotic lesions, prepared a dexamethasone palmitate (
DP)-LDL complex, and examined the effect of the DP-LDL complex on foam cell
formation of macrophages in vitro. LDL was isolated from human plasma and
the DP-LDL complex was prepared by incubation in the presence of Celite 545
. The complex contained about 50 mol of DP in 1 mol of LDL. When macrophage
s were incubated with LDL for 48 h, cholesterol eater was accumulated in th
e macrophages, indicating foam cell formation. This accumulation of cholest
erol ester was significantly inhibited by incubation with the DP-LDL comple
x. The potency of the DP-LDL complex was similar to that of dexamethasone a
lone. The DP-LDL complex also significantly attenuated the accumulation of
cholesterol ester induced by incubation with LDL prior to the incubation wi
th the DP-LDL complex. These findings indicated that the DP-LDL complex sho
wed similar characteristics to LDL, and the DP-LDL complex inhibited the fo
am cell formation of macrophages in in vitro experiments. This DP-LDL compl
ex has a possibility as a drug-carrier complex for use in atherosclerosis.